Losartan-Vertex pills 50mg, 30pcs

Composition

Active ingredient:

 Losartan potassium 50 mg;

Auxiliary substances:

MCC;

mannitol;

croscarmellose sodium;

povidone 30;

magnesium stearate;

hypromellose;

titanium dioxide;

talc;

propylene

glycol Pharmacological action

Losartan is a specific oral angiotensin II receptor antagonist (tina AT1). Angiotensin II selectively binds to AT1 receptors found in many tissues (vascular smooth muscle, adrenal glands, kidneys, and heart) and performs several important biological functions, including vasoconstriction and aldosterone release. Angiotensin II also stimulates smooth muscle cell proliferation.

Losartan and its pharmacologically active metabolite (E 3174) both in vitro and in vivo block all physiological effects of angiotensin II, regardless of the source or route of synthesis. Losartan selectively binds to AT1 receptors: it does not bind or block the receptors of other hormones and ion channels that play an important role in regulating the function of the cardiovascular system. In addition, losartan does not inhibit the angiotensin-converting enzyme (ACE), which contributes to the degradation of bradykinin, so side effects indirectly associated with bradykinin (for example, angioedema) are quite rare.

When losartan is used, the absence of negative feedback on renin secretion leads to an increase in plasma renin activity. An increase in renin activity leads to an increase in the concentration of angiotensin II in blood plasma. However, antihypertensive activity and a decrease in plasma aldosterone concentration remain, which indicates an effective blockade of angiotensin II receptors. After discontinuation of losartan, plasma renin activity and angiotensin II concentration decreased for 3 days to the initial values observed before starting the drug.

Losartan and its active metabolite have a high affinity for angiotensin II (type AT1) receptors.

The plasma concentrations of losartan and its active metabolite, as well as the antihypertensive effect of losartan, increase with increasing dose.

The maximum antihypertensive effect develops in 3-6 weeks after the start of taking the drug.

In patients with arterial hypertension, proteinuria (more than 2 g per day), without diabetes mellitus, the use of the drug significantly reduces proteinuria, albumin and immunoglobulin G (IgG) excretion.

In post-menopausal women with arterial hypertension who took losartan at a dose of 50 mg / day for 4 weeks, no effect of therapy on renal and systemic prostaglandin levels was found.

Losartan has no effect on autonomic reflexes and does not have a long-term effect on the level of norepinephrine in blood plasma.

In patients with arterial hypertension, losartan at doses up to 150 mg per day does not cause clinically significant changes in the concentration of triglycerides, total cholesterol and high-density lipoprotein cholesterol. In the same doses, losartan does not affect the concentration of glucose in the fasting blood. Losartan caused a decrease in the serum uric acid concentration (usually less than 0.4 mg / dl), which persisted during long-term therapy. In controlled clinical trials involving patients with arterial hypertension, there were no cases of drug withdrawal due to an increase in serum creatinine or potassium.

Pharmacokinetics

Suction

When taken orally, losartan is well absorbed from the gastrointestinal tract. The systemic bioavailability of losartan is approximately 33%, and food intake does not affect the bioavailability of losartan. The average maximum concentrations of losartan and its active metabolite are reached after 1 h and after 3-4 h, respectively.

Distribution

Losartan and its active metabolite bind to plasma proteins (mainly albumin) by more than 99%. The volume of distribution of losartan is 34 l. Losartan practically does not penetrate the blood-brain barrier.

Metabolism

Losartan undergoes the effect of “primary passage” through the liver, is megabolized with the participation of the cytochrome P450 isoenzyme CYP2C9. Approximately 14% of the dose of losartan administered intravenously or orally is converted to its active metabolite (EXP3174) with a carboxyl group. Biologically inactive metabolites are also formed: two main ones (as a result of hydroxylation of the butyl side chain) and a less significant one-N-2-tetrazole-glucuronide.

Deduction

The plasma clearance of losartan and its active metabolite is 600 ml / min and 50 ml/min, respectively. The renal clearance of losartan and its active metabolite is approximately 74 ml / min and 26 ml / min, respectively. When taking losartan orally, about 4% of the dose is excreted unchanged by the kidneys and within 6% of the dose is excreted by the kidneys as an active metabolite. Losartan and its active metabolite have linear pharmacokinetics when taking losartan orally at doses up to 200 mg. After oral use, plasma concentrations of losartan and its active metabolite decrease polyexponentially with a final T1/2 of approximately 2 and 6-9 hours, respectively.

The elimination of losartan and its metabolites occurs in the bile and kidneys. After oral use of losartan labeled with 14C, about 35% of the radioactive label is detected in the urine and 58% in the feces.

Pharmacokinetics in special patient groups

The plasma concentrations of losartan and its active metabolite in elderly male patients with arterial hypertension do not significantly differ from those in younger male patients with arterial hypertension.

Plasma concentrations of losartan were 2 times higher in women with arterial hypertension compared to men with arterial hypertension. Concentrations of the active metabolite did not differ between men and women. This apparent pharmacokinetic difference is not clinically relevant.

When taking losartan orally, the concentrations of losartan and its active metabolite in the blood plasma of Nazis with alcoholic cirrhosis of mild and moderate severity were 5 and 1.7 times higher (respectively) than in young healthy male and female volunteers.

Plasma concentrations of losartan in patients with creatinine clearance above 10 ml / min did not differ from those in patients with normal renal function. In patients requiring hemodialysis, the area under the concentration-time curve (AUC) is approximately 2 times larger than in patients with normal renal function. Plasma concentrations of the active metabolite do not change in patients with impaired renal function or in patients undergoing hemodialysis. Losartan and its active metabolite are not removed from the bloodstream by hemodialysis.

Indications

• Arterial hypertension;
• congestive heart failure (as part of combination therapy, in case of intolerance or failure of therapy with ACE inhibitors);
• the reduction in the risk of stroke in patients with hypertension and left ventricular hypertrophy;
• protection of renal function in patients with diabetes mellitus type 2 with proteinuria with the aim of reducing proteinuria, reduce the progression of kidney damage, reduce the risk of end-stage (to prevent the need for dialysis, the probability of an increase in creatinine in the blood serum).

Contraindications

Hypersensitivity, pregnancy, breast-feeding.

Side effects

Nervous system and sensory disorders:  ≥1% — dizziness, asthenia/fatigue, headache, insomnia;

Respiratory system disorders:  ≥1% — nasal congestion, cough, upper respiratory tract infections (fever, sore throat, etc. ), sinusopathy, sinusitis, pharyngitis;

From the digestive tract:  ≥1% — nausea, diarrhea, dyspeptic symptoms, abdominal pain;

From the musculoskeletal system:  ≥1% — cramps, myalgia, back pain, chest pain, and leg pain.

Cardiovascular and blood disorders (hematopoiesis, hemostasis):  <1% — orthostatic reaction (dose-dependent), hypotension, palpitations, a tachy or bradycardia, arrhythmia, angina, anemia.

From the genitourinary system:  <1% — of the imperative urge to urinate, urinary tract infections, impaired kidney function, weakening of libido, impotence.

From the side of the skin:  <1% — dry skin, erythema, blood flow, photosensitivity, sweating, alopecia.

Allergic reactions:  <1% — hives, rash, itching, angioedema, including the face, lips, pharynx and/or tongue.

Other services:  ≥1% – hyperkalemia.

How to take it, course of use and dosage

Losartan is taken orally, for adults, regardless of food intake,1 time a day.

With arterial hypertension-50 mg, if necessary, a gradual increase in the dose is possible (in some cases up to the maximum daily dose of 100 mg).

In chronic heart failure — 12.5 mg with a gradual increase in 2 stages (after 1 week – up to 25 mg and after another 1 week-50 mg) to the usual maintenance dose of 50 mg.

Composition

Tablet Form of production

Storage conditions

Store in a dry place, protected from light, at a temperature not exceeding 25 °C.

Active ingredient

Losartan

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

For adults as directed by your doctor

Indications

Hypertension, Prevention of heart attacks and strokes, Diabetic nephropathy, Heart failure